IL234486A - Piazolo-based compounds [a – 5,1] pyrimidine - Google Patents
Piazolo-based compounds [a – 5,1] pyrimidineInfo
- Publication number
- IL234486A IL234486A IL234486A IL23448614A IL234486A IL 234486 A IL234486 A IL 234486A IL 234486 A IL234486 A IL 234486A IL 23448614 A IL23448614 A IL 23448614A IL 234486 A IL234486 A IL 234486A
- Authority
- IL
- Israel
- Prior art keywords
- mmol
- pyrimidin
- pyrazolo
- nmr
- reaction
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261608765P | 2012-03-09 | 2012-03-09 | |
| PCT/US2013/029056 WO2013134228A1 (en) | 2012-03-09 | 2013-03-05 | PYRAZOLO[1,5-a]PYRIMIDINE-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IL234486A true IL234486A (en) | 2016-10-31 |
Family
ID=47892052
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL234486A IL234486A (en) | 2012-03-09 | 2014-09-07 | Piazolo-based compounds [a – 5,1] pyrimidine |
Country Status (26)
| Country | Link |
|---|---|
| US (3) | US8946415B2 (ja) |
| EP (1) | EP2834243B1 (ja) |
| JP (1) | JP6418950B2 (ja) |
| KR (1) | KR101965025B1 (ja) |
| CN (1) | CN104302649B (ja) |
| AR (1) | AR090292A1 (ja) |
| AU (1) | AU2013230128B2 (ja) |
| BR (1) | BR112014022000A8 (ja) |
| CA (1) | CA2866143C (ja) |
| DK (1) | DK2834243T3 (ja) |
| ES (1) | ES2676224T3 (ja) |
| HK (1) | HK1201257A1 (ja) |
| HU (1) | HUE038786T2 (ja) |
| IL (1) | IL234486A (ja) |
| IN (1) | IN2014DN07384A (ja) |
| MX (1) | MX345830B (ja) |
| NZ (1) | NZ630721A (ja) |
| PL (1) | PL2834243T3 (ja) |
| PT (1) | PT2834243T (ja) |
| RU (1) | RU2014140735A (ja) |
| SG (1) | SG11201405561RA (ja) |
| TR (1) | TR201808280T4 (ja) |
| TW (1) | TW201341386A (ja) |
| UY (1) | UY34668A (ja) |
| WO (1) | WO2013134228A1 (ja) |
| ZA (1) | ZA201406149B (ja) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ630721A (en) | 2012-03-09 | 2016-12-23 | Lexicon Pharmaceuticals Inc | Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use |
| ES2676826T3 (es) | 2012-03-09 | 2018-07-25 | Lexicon Pharmaceuticals, Inc. | Compuestos basados en imidazo[1,2-b]piridazina, composiciones que los comprenden y usos de los mismos |
| US8901305B2 (en) | 2012-07-31 | 2014-12-02 | Bristol-Myers Squibb Company | Aryl lactam kinase inhibitors |
| CN105121445A (zh) | 2013-02-22 | 2015-12-02 | 百时美施贵宝公司 | 作为连接蛋白相关激酶1(AAK1)抑制剂的5H-色烯并[3,4-c]吡啶 |
| TW201542550A (zh) | 2013-09-06 | 2015-11-16 | Lexicon Pharmaceuticals Inc | 吡唑并［１，５－ａ］嘧啶基化合物、包含彼之組合物以及使用彼之方法 |
| CN105979950A (zh) | 2013-10-11 | 2016-09-28 | 百时美施贵宝公司 | 吡咯并三嗪激酶抑制剂 |
| HRP20221518T1 (hr) | 2014-01-24 | 2023-02-17 | Turning Point Therapeutics, Inc. | Diaril makrociklični spojevi kao modulatori protein kinaza |
| EP3099673B1 (en) * | 2014-01-31 | 2018-09-26 | Bristol-Myers Squibb Company | Quinoline-based kinase inhibitors |
| TW201620911A (zh) * | 2014-03-17 | 2016-06-16 | 雷西肯製藥股份有限公司 | 銜接子關聯激酶１之抑制劑、包含其之組成物、及其使用方法 |
| EP3200797A1 (en) * | 2014-09-30 | 2017-08-09 | Bristol-Myers Squibb Company | Quinazoline-based kinase inhibitors |
| EP4420732A2 (en) * | 2014-12-15 | 2024-08-28 | CMG Pharmaceutical Co., Ltd. | Fused ring heteroaryl compounds and their use as trk inhibitors |
| US10174044B2 (en) | 2015-04-10 | 2019-01-08 | Bristol-Myers Squibb Company | Fused pyridines as kinase inhibitors |
| MX2017017097A (es) | 2015-07-02 | 2018-05-23 | Tp Therapeutics Inc | Macrociclos diarílicos quirales como moduladores de proteínas quinasas. |
| PT3319969T (pt) | 2015-07-06 | 2024-06-17 | Turning Point Therapeutics Inc | Polimorfo de macrociclo de diarilo |
| RU2020123800A (ru) | 2015-07-21 | 2020-10-02 | Тёрнинг Поинт Терапьютикс, Инк. | Хиральные диарильные макроциклы и их применение |
| AU2016348549B2 (en) | 2015-11-02 | 2020-07-23 | Janssen Pharmaceutica Nv | [1,2,4]triazolo[1,5-a]pyrimidin-7-yl compound |
| BR112019001607A2 (pt) | 2016-07-28 | 2019-04-30 | Tp Therapeutics, Inc. | inibidores macrocíclicos de quinases |
| EA039102B1 (ru) | 2016-11-02 | 2021-12-03 | Янссен Фармацевтика Нв | Соединения [1,2,4]триазоло[1,5-a]пиримидина в качестве ингибиторов pde2 |
| CA3038913A1 (en) | 2016-11-02 | 2018-05-11 | Janssen Pharmaceutica Nv | [1,2,4]triazolo[1,5-a]pyrimidine compounds as pde2 inhibitors |
| CN109923116B (zh) | 2016-11-02 | 2022-12-06 | 詹森药业有限公司 | 作为pde2抑制剂的[1,2,4]三唑并[1,5-a]嘧啶衍生物 |
| TWI808958B (zh) | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| PT3658557T (pt) | 2017-07-28 | 2024-09-11 | Nimbus Lakshmi Inc | Inibidores de tyk2 e usos dos mesmos |
| PT3658148T (pt) | 2017-07-28 | 2024-08-26 | Turning Point Therapeutics Inc | Compostos macrocíclicos e utilizações dos mesmos |
| MX2020006490A (es) | 2017-12-19 | 2020-08-17 | Turning Point Therapeutics Inc | Compuestos macrociclicos para tratar enfermedades. |
| WO2019120194A1 (zh) * | 2017-12-22 | 2019-06-27 | 深圳市塔吉瑞生物医药有限公司 | 一种取代的吡唑并[1,5-a]嘧啶化合物及其药物组合物及用途 |
| WO2019144885A1 (zh) | 2018-01-23 | 2019-08-01 | 深圳市塔吉瑞生物医药有限公司 | 取代的吡唑并[1,5-a]嘧啶类的大环化合物 |
| US20220041588A1 (en) * | 2018-09-27 | 2022-02-10 | Fochon Pharmaceuticals, Ltd. | Substituted imidazo[1,2-a]pyridine and [1,2,4]triazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
| EP3866789A4 (en) * | 2018-10-15 | 2022-07-06 | Nimbus Lakshmi, Inc. | TYK2 INHIBITORS AND USES THEREOF |
| EP4138844A1 (en) * | 2020-04-21 | 2023-03-01 | Lexicon Pharmaceuticals, Inc. | 4-(3-(pyridin-3-yl)pyrazolo[1,5-a]pyrimidin-5-yl)piperazine for use in the the treatment of cov-229e or cov-oc43 coronaviruses infections |
| JP2023522688A (ja) | 2020-04-21 | 2023-05-31 | レクシコン ファーマシューティカルズ インコーポレイテッド | ウイルス感染症の治療に使用されるａａｋ１阻害剤 |
| US11478733B2 (en) | 2020-11-24 | 2022-10-25 | Caterpillar Inc. | Filter interlock with tabs mating with a pedestal or a housing |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5464764A (en) | 1989-08-22 | 1995-11-07 | University Of Utah Research Foundation | Positive-negative selection methods and vectors |
| AU2515992A (en) | 1991-08-20 | 1993-03-16 | Genpharm International, Inc. | Gene targeting in animal cells using isogenic dna constructs |
| US6194410B1 (en) * | 1998-03-11 | 2001-02-27 | Hoffman-La Roche Inc. | Pyrazolopyrimidine and pyrazolines and process for preparation thereof |
| JP4847275B2 (ja) * | 2005-10-21 | 2011-12-28 | 田辺三菱製薬株式会社 | ピラゾロ［１，５−ａ］ピリミジン化合物 |
| ATE502943T1 (de) | 2006-09-29 | 2011-04-15 | Novartis Ag | Pyrazolopyrimidine als pi3k-lipidkinasehemmer |
| US20120058997A1 (en) * | 2006-11-06 | 2012-03-08 | Supergen, Inc. | Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors |
| MX2010012457A (es) * | 2008-05-13 | 2010-12-07 | Irm Llc | Heterociclos que contienen nitrogeno fusionado y composiciones de los mismos como inhibidores de cinasa. |
| BRPI0919873B8 (pt) * | 2008-10-22 | 2021-05-25 | Array Biopharma Inc | compostos de pirazol[1,5-a]pirimidina substituídos como inibidores da trk quinase, seus processos de preparação e composições farmacêuticas |
| AR077468A1 (es) * | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| US8865726B2 (en) | 2009-09-03 | 2014-10-21 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrimidine compounds as mTOR inhibitors |
| EP2523552B1 (en) * | 2010-01-14 | 2015-05-13 | Merck Sharp & Dohme Corp. | Pyrazolo[1,5-a]pyrimidines as mark inhibitors |
| WO2013013188A1 (en) * | 2011-07-21 | 2013-01-24 | Tolero Pharmaceuticals, Inc. | Heterocyclic protein kinase inhibitors |
| NZ630721A (en) | 2012-03-09 | 2016-12-23 | Lexicon Pharmaceuticals Inc | Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use |
| EP3235499A3 (en) | 2012-03-09 | 2018-01-17 | Lexicon Pharmaceuticals, Inc. | Inhibition of adaptor associated kinase 1 for the treatment of pain |
| ES2676826T3 (es) | 2012-03-09 | 2018-07-25 | Lexicon Pharmaceuticals, Inc. | Compuestos basados en imidazo[1,2-b]piridazina, composiciones que los comprenden y usos de los mismos |
| TW201620911A (zh) * | 2014-03-17 | 2016-06-16 | 雷西肯製藥股份有限公司 | 銜接子關聯激酶１之抑制劑、包含其之組成物、及其使用方法 |
-
2013
- 2013-03-05 NZ NZ630721A patent/NZ630721A/en unknown
- 2013-03-05 EP EP13710250.5A patent/EP2834243B1/en active Active
- 2013-03-05 DK DK13710250.5T patent/DK2834243T3/en active
- 2013-03-05 SG SG11201405561RA patent/SG11201405561RA/en unknown
- 2013-03-05 AU AU2013230128A patent/AU2013230128B2/en active Active
- 2013-03-05 BR BR112014022000A patent/BR112014022000A8/pt not_active Application Discontinuation
- 2013-03-05 US US13/785,355 patent/US8946415B2/en active Active
- 2013-03-05 ES ES13710250.5T patent/ES2676224T3/es active Active
- 2013-03-05 MX MX2014010589A patent/MX345830B/es active IP Right Grant
- 2013-03-05 KR KR1020147028071A patent/KR101965025B1/ko active IP Right Grant
- 2013-03-05 TR TR2018/08280T patent/TR201808280T4/tr unknown
- 2013-03-05 IN IN7384DEN2014 patent/IN2014DN07384A/en unknown
- 2013-03-05 HU HUE13710250A patent/HUE038786T2/hu unknown
- 2013-03-05 JP JP2014561024A patent/JP6418950B2/ja active Active
- 2013-03-05 PL PL13710250T patent/PL2834243T3/pl unknown
- 2013-03-05 WO PCT/US2013/029056 patent/WO2013134228A1/en active Application Filing
- 2013-03-05 CA CA2866143A patent/CA2866143C/en active Active
- 2013-03-05 PT PT137102505T patent/PT2834243T/pt unknown
- 2013-03-05 RU RU2014140735A patent/RU2014140735A/ru not_active Application Discontinuation
- 2013-03-05 CN CN201380012483.0A patent/CN104302649B/zh active Active
- 2013-03-08 TW TW102108283A patent/TW201341386A/zh unknown
- 2013-03-11 UY UY0001034668A patent/UY34668A/es not_active Application Discontinuation
- 2013-03-11 AR ARP130100765A patent/AR090292A1/es unknown
-
2014
- 2014-08-21 ZA ZA2014/06149A patent/ZA201406149B/en unknown
- 2014-09-07 IL IL234486A patent/IL234486A/en active IP Right Grant
- 2014-09-11 US US14/483,898 patent/US9403832B2/en active Active
-
2015
- 2015-02-13 HK HK15101651.1A patent/HK1201257A1/xx unknown
-
2016
- 2016-07-12 US US15/207,677 patent/US20170129896A1/en not_active Abandoned
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FF | Patent granted | ||
| KB | Patent renewed | ||
| KB | Patent renewed |